Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
Type:
Grant
Filed:
May 28, 2009
Date of Patent:
December 20, 2011
Assignees:
North Carolina State University, Zettacore, Inc.
Inventors:
Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
Abstract: Compounds according to formula (I): wherein A, R1 and R2 are as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof are useful for the modulation of CCR5 chemokine receptor activity.
Type:
Grant
Filed:
December 9, 2005
Date of Patent:
December 13, 2011
Assignee:
Virochem Pharma Inc.
Inventors:
Laval Chan Chun Kong, Christophe Moinet, Marc Courchesne, Louis Vaillancourt, Monica Bubenik
Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
Abstract: A process for the preparation of trityl olmesartan comprising (a) condensing 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazol-5-carboxylic acid alkyl ester with trityl biphenyl bromide in the presence of a polar aprotic solvent and a base selected from the group consisting of alkali metal carbonates, alkali metal hydroxides, alkali metal alkoxides, and tertiary amines to obtain a compound of formula V, b) deesterifying the compound of formula (V) with a base; and c) reacting the product of step (b) with 4-halomethyl-5-methyl-2-oxo-1,3-dioxolene of formula (IV), wherein X is halogen selected from F or Cl or Br or I, to obtain trityl olmesartan medoxomil of formula. The trityl olmesartan medoxomil may be deprotected to produce olmesartan medoxomil.
Abstract: Embodiments of the present subject matter provide a compound and material that may be used as a lead-free primary explosive. An embodiment of the present subject matter provides the compound copper(I) nitrotetrazolate. Certain embodiments of the present subject matter provide methods for preparing lead-free primary explosives. The method includes: providing cuprous salt; providing water; providing 5-nitrotetrazolate salt; combining the cuprous salt, water and 5-nitrotetrazolate salt to form a mixture; and heating the mixture. The method may also include providing cuprous chloride and providing sodium 5-nitrotetrazolate. Certain embodiments of the present subject matter also provide methods for preparing copper(I) nitrotetrazolate. The method includes: providing cuprous salt; providing water; providing 5-nitrotetrazolate salt; combining the cuprous salt, water and 5-nitrotetrazolate salt to form a mixture; and heating the mixture.
Type:
Grant
Filed:
October 8, 2010
Date of Patent:
December 6, 2011
Assignee:
Pacific Scientific Energetic Materials Company
Inventors:
John W. Fronabarger, Michael D. Williams, William B Sanborn
Abstract: There is provided compounds of formula I, wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
Type:
Grant
Filed:
April 12, 2006
Date of Patent:
November 29, 2011
Assignee:
Vicore Pharma AB
Inventors:
Mathias Alterman, Anders Hallberg, Xiongyu Wu
Abstract: The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.
Type:
Grant
Filed:
May 7, 2008
Date of Patent:
November 22, 2011
Assignee:
Eli Lilly and Company
Inventors:
Joyce Z. Crich, James Robert Henry, Hong Hu, Delu Jiang, Hong-Yu Li, William Thomas McMillen, Jason Scott Sawyer, Melissa Kate Slater, Yan Wang
Abstract: The present invention relates to triazole derivaties, a method for the preparation thereof, and a pharmaceutical composition containing the same as an active ingredient. The inventive triazole derivaties have an excellent antifungal activity against various pathogens.
Type:
Grant
Filed:
December 28, 2007
Date of Patent:
November 22, 2011
Assignee:
Daewoong Pharmaceutical Co., Ltd.
Inventors:
Joon Seok Park, Kyung A Yu, Yun Soo Yoon, Mi Ryeong Han
Abstract: The present invention relates to Compounds represented by the formula (I) or salts thereof. In the formula (I), the ring A represents a benzene ring, a thiophene ring, or a pyridine ring; Ra represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group; the ring B represents a pyridine ring, a pyrimidine ring, or a quinoline ring; the ring C represents a benzene ring; a pyridine ring, a quinoline ring, or an isoquinoline ring; X and Y, the same or different, represent an oxygen atom or a sulfur atom, with the proviso that the case X is a sulfur atom and Y is an oxygen atom be excluded; R1 represents a hydrogen atom, a halogen atom, an amino group, a cycloalkylamino group, an alkylcarbonylamino group, an alkyloxycarbonylamino group, an alkylaminocarbonyl group, or a non-aromatic heterocyclic group; and R2 and R2?, the same or different, represent a hydrogen atom, a halogen atom, an alkyl group, a halogeno-alkyl group, or a halogeno-alkoxy group.
Type:
Grant
Filed:
January 29, 2008
Date of Patent:
November 22, 2011
Assignee:
Santen Pharmaceutical Co., Ltd.
Inventors:
Takahiro Honda, Koushi Fujisawa, Hiroyuki Aono, Masakazu Ban
Abstract: Methods of preparing heterocyclic triazolium-based nitrate salts by a streamlined process are provided. Such salts offer energetic performance as well as pharmaceutical potential.
Type:
Grant
Filed:
October 12, 2010
Date of Patent:
November 22, 2011
Assignee:
The United States of America as represented by the Secretary of the Air Force
Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
Type:
Grant
Filed:
August 13, 2007
Date of Patent:
November 22, 2011
Assignees:
Novartis AG, Xenon Pharmaceuticals Inc.
Abstract: The present invention provides new tyrphostin derivatives acting as substrate competitive protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PTK and RTK related disorders such as metabolic, fibrotic, and cell proliferative disorders, in particular psoriasis and cancer.
Type:
Grant
Filed:
December 4, 2007
Date of Patent:
November 15, 2011
Assignee:
Novotyr Therapeutics Ltd.
Inventors:
Hadas Reuveni, Alexander Levitzki, Lilach Steiner, Revital Sasson, Iris Ben-David, Avi Weissberg
Abstract: The present invention discloses two new related substances (6) and (7) of Anastrozole synthesis from Q.A. Salt (5) as in Scheme—1 and purification procedures to get Anastrozole (1) free from (6) and (7).
Abstract: Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.
Type:
Grant
Filed:
October 5, 2006
Date of Patent:
November 8, 2011
Assignee:
Exelixis, Inc.
Inventors:
Patrick Kearney, S. David Brown, Elena S. Koltun
Abstract: A cross-linked polyisocyanate polymer and a process for preparation of a polymer having the general structure (I) including reacting an effective amount of tetrazole polyol with isocyanate resin, combining at a temperature in the range of about 50° C. to about 100° C. for a time period in the range of about 1 to about 24 hours and cooling to room temperature producing a cross-linked polyisocyanate polymer.
Type:
Grant
Filed:
September 26, 2008
Date of Patent:
November 8, 2011
Assignee:
The United States of America as represented by the Secretary of the Navy
Abstract: A composition for use in making commercial food and skin products comprising S-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.
Type:
Grant
Filed:
September 14, 2009
Date of Patent:
November 1, 2011
Assignees:
Australian Health & Nutrition Assoc. Ltd., Children's Hospital Medical Center
Inventors:
Kenneth David Reginald Setchell, Sidney John Cole
Abstract: The invention relates to the use of compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,4-triazole derivatives of formula (I) to processes of preparation of such compounds and to pharmaceutical compositions comprising them.
Type:
Grant
Filed:
November 7, 2007
Date of Patent:
October 18, 2011
Assignee:
Laboratorios Del Dr. Esteve, S.A.
Inventors:
Nadine Jagerovic, Jose Maria Cumella-Montanchez, Maria Pilar Goya-Laza, Alberto Dordal Zueras, Maria Rosa Cuberes-Altisent
Abstract: (2S)-[4-(Carboxymethyl)thiazol-2-ylthio]-N-{[4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}acetamide hydrobromide and a crystal thereof, which resist easy weight change caused by vapor sorption as compared to a free form, and are superior as drug substances of pharmaceutical products, and a production intermediate therefor are provided.
Abstract: A process for the preparation of ?-alkoxycarbonylamino-?-aminoacids and ?,? orthogonally diprotected diaminoacids from ?,?-diaminoacids using 1-alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ?-alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ?-alkoxycarbonylamino-?-aminoacids with benzotriazoles are also disclosed.
Type:
Grant
Filed:
August 4, 2006
Date of Patent:
September 27, 2011
Assignee:
F.I.S. Fabbrica Italiana Sintetici S.p.A.
Inventors:
Siro Serafini, Riccardo Motterle, Elena Brasola
Abstract: A compound represented by the general formula (I): (I) wherein R represents linear, branched, or cyclic alkyl or aryl; a process for producing the compound; and an antitumor agent containing the compound as an active ingredient.